Evidence map›Paper›PMID 37033416›Full record

ArticleEuropean journal of medicinal chemistry reports2023

Chalcone: A potential scaffold for NLRP3 inflammasome inhibitors.

Pritam Thapa, Sunil P Upadhyay, Vikas Singh, Varun C Boinpelly, Jianping Zhou, David K Johnson, Prajwal Gurung, Eung Seok Lee, Ram Sharma, Mukut Sharma

Abstract read
In one paragraph

Article in European journal of medicinal chemistry reports, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

16 citing papers in PubMed.

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  8. Discovery of (Molecules (Basel, Switzerland) · 2025
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Pritam ThapaDrug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO, 64128, USA.
Sunil P UpadhyayDrug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO, 64128, USA.
Vikas SinghDivision of Neurology, KCVA Medical Center, Kansas City, MO, USA.
Varun C BoinpellyRenal Research Laboratory, Kansas City VA Medical Center, Kansas City, MO, USA.
Jianping ZhouRenal Research Laboratory, Kansas City VA Medical Center, Kansas City, MO, USA.
David K JohnsonDepartment of Computational Chemical Biology Core, Molecular Graphics and Modeling Core, University of Kansas, KS, 66047, USA.
Prajwal GurungInflammation Program, University of Iowa, Iowa City, IA, 52242, USA.
Eung Seok LeeCollege of Pharmacy, Yeungnam University, Gyeongsan, 712-749, Republic of Korea.
Ram SharmaDrug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO, 64128, USA.
Mukut SharmaDrug Discovery Program, Midwest Veterans' Biomedical Research Foundation, KCVA Medical Center, Kansas City, MO, 64128, USA.

Funding

Synthetic Chemical Biology CoreP20GM113117 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI OROZCO, ROBIN C. · 2016 to 2025
$23.9M
Implicating a previously unknown Dectin1-RIPK2-CARD9 signaling in providing resistance against Leishmania major infectionR01AI155425 · NIAID · UNIVERSITY OF IOWA · PI GURUNG, PRAJWAL · 2021 to 2025
$2.5M
NIAID NIH HHS R01 AI155425NIGMS NIH HHS P20 GM113117
6 · The paper itself

Abstract

Overactivated NLRP3 inflammasome has been shown to associate with an increasing number of disease conditions. Activation of the NLRP3 inflammasome results in caspase-1-catalyzed formation of active pro-inflammatory cytokines (IL-1β and IL-18) resulting in pyroptosis. The multi-protein composition of the NLRP3 inflammasome and its sensitivity to several damage-associated molecular patterns (DAMPs) and pathogen-associated molecular patterns (PAMPs) make this extensively studied inflammasome an attractive target to treat chronic conditions. However, none of the known NLRP3 inhibitors has been approved for clinical use. Sulfonylurea and covalent inhibitors with electrophilic warhead (Michael acceptor) are among the prominent classes of compounds explored for their NLRP3 inhibitory effects. Chalcone, a small molecule with α, β unsaturated carbonyl group (Michael acceptor), has also been studied as a promising scaffold for the development of NLRP3 inhibitors. Low molecular weight, easy to manipulate lipophilicity and cost-effectiveness have attracted many to use chalcone scaffold for drug development. In this review, we highlight chalcone derivatives with NLRP3 inflammasome inhibitory activities. Recent developments and potential new directions summarized here will, hopefully, serve as valuable perspectives for investigators including medicinal chemists and drug discovery researchers to utilize chalcone as a scaffold for developing novel NLRP3 inflammasome inhibitors.

Indexed as

ChalconeMichael acceptorsNLRP3 inflammasomeNLRP3 inhibitorsSulfonylureas

Identifiers

PMID37033416
PMCPMC10081147

What OpenQuestion holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.